Thiethylperazine dimaleate is a phenothiazine derivate, and an orally active dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a slective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects[1][2][3].
Pomalidomide-amino-PEG4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology[1].
Midostaurin (CGP41231; PKC412) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50 ranging from 16-500 nM.
THP-PEG4-Pyrrolidine(N-Me)-CH2OH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523)[1].
Flufenamic acid-d4 is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
Camelliaside A is a flavonoid from the methanol extract of tea (Camellia oleifera) seed pomace[1].
5’-O-(4,4’-Dimethoxytrityl)-N6-phenoxyacetyl adenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively[1].
Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib is a drug for the treatment of ER-positive and HER2-negative breast cancer.
AH23848 hemicalcium salt is a potent, specific and orally active thromboxane receptor blocker. AH23848 hemicalcium salt inhibits platelet deposition[1].
Antibacterial agent 129, an oxetanyl-quinoline derivative, has shown good antibacterial activity against P. mirabilis and B. subtilis with MICs of 31.25 μM and 31.5 μM and . Antibacterial agent 129 shows good antifungal activity against A. niger with a MIC of 31.25 μM. Antibacterial agent 129 shows excellent antimycobacterial activity with MIC 57.73 μM for M. tuberculosis H37Rv[1].
Allethrin, a pyrethroid insecticide is a major mosquito repellent agent. Allethrin induces oxidative stress, apoptosis and calcium release in rat testicular carcinoma cells (LC540). Allethrin induces BCL-2, caspase-3 activation and release of intracellular calcium[1].
MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range.
LDN-27219 is a potent inhibitor of hTGase(Tissue transglutaminase) with an IC50 of 0.6 uM.IC50 value: 0.6 uM [1]Target: hTGase inhibitorLDN-27219 is a potent inhibitor of the enzyme(hTGase), producing 100% inhibition at the screening concentration of 10 uM. To examine the enzyme selectivity of LDN-27219, it was tested as an inhibitor of coagulation Factor XIIIa and caspase 3. At concentrations as high as 50 íM, the compound had no effect on the activities of either of these enzymes. LDN-27219 was found to be nontoxic at concentrations as high as 100 íM in an assay that measures the viability of HT1080 cells, a fibrosarcoma tumor cell line.
FMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay.
Milbemycin oxime is a veterinary drug from the group of milbemycins, used as a broad spectrum antiparasitic.
Amlodipine aspartic acid impurity is the impurity of Amlodipine aspartic acid. Amlodipine aspartic acid is a calcium channel blocker with antihypertensive and antianginal properties.
Irpagratinib (ABSK011) is an orally active inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinase, targeting to FGFR4 (IC50<10 nM). Irpagratinib inhibits the auto-phosphorylation of FGFR4 and blocks signal transduction from FGFR4 to downstream pathway activation. Irpagratinib exhibits high exposure in PK study in mouse, rat and dog, and also shows antineoplastic/anti-tumor activity in subcutaneous xenograft tumor models[1].
Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation.
Isoapetalic acid (compound 4) is a potent anti-HIV agent[1].
12α-Hydroxygrandiflorenic acid is a compound isolated from the whole plant of Wedelia chinensis (Osbeck.)[1].
USP1-IN-4 (compound 10) is an effective USP1 inhibitor with an IC50 value of 2.44 nM. USP1-IN-4 has anticancer activity and synergistic activity with various anticancer drugs[1].
Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.
Carteolol is a non-selective β-adrenoceptor antagonist. Carteolol induces apoptosis via a caspase activated and mitochondrial-dependent pathway. Carteolol can be used for glaucoma research[1].
1-(3’-O-[4,4’-Dimethoxytrityl]-alpha-L-threofuranosyl)-thymine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Poziotinib(NOV120101; HM781-36B) is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively.IC50 value: 3/5/23 nM(HER1/HER2/HER4) [1]Target: pan-HER inhibitorin vitro: The IC50 levels of HM781-36B for N87 and SNU216 were 0.001 and 0.004 μmol/L, respectively, which was 10–1000 fold lower than the IC50 levels of other HER family TKIs. HM781-36B more potently inhibited the phosphorylation of HER family and downstream proteins, and induced apoptosis and G1 arrest compared to gefitinib or lapatinib [1]. HM781-36B is a potent inhibitor of EGFR in vitro, including the EGFR-acquired resistance mutation (T790M), as well as HER-2 and HER-4, compared with other EGFR tyrosine kinases inhibitors (erlotinib, lapatinib and BIBW2992). HM781-36B treatment of EGFR DelE746_A750-harboring erlotinib-sensitive HCC827 and EGFR L858R/T790M-harboring erlotinib-resistant NCI-H1975 NSCLC cells results in the inhibition of EGFR phosphorylation and the subsequent deactivation of downstream signaling proteins [2]. The addition of HM781-36B induced potent growth inhibition in both DiFi cells with EGFR overexpression and SNU-175 cells (IC50 = 0.003 and 0.005 μM, respectively). Furthermore, HM781-36B induced G1 arrest of the cell cycle and apoptosis, and reduced the levels of HER family and downstream signaling molecules, pERK and pAKT, as well as nonreceptor/cytoplasmic tyrosine kinase, BMX [3].in vivo: The growth of tumors in mice treated with HM781-36B alone or in combination with 5-FU was significantly inhibited compared with control mice, and tumor volume in mice receiving coadministraion of HM781-36B and 5-FU was smaller than tumor volume in mice receiving HM781-36B only [1].
E3 ligase Ligand-Linker Conjugates 5 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.
AEOL-10150 pentachloride is a metalloporphyrin catalytic antioxidant and is a superoxide dismutase mimetic, and protects lungs from radiation-induced injury[1].
Trifluralin is a commonly used pre-emergence herbicide. Trifluralin is generally applied to the soil to provide control of a variety of annual grass and broadleaf weed species. It inhibits root development by interrupting mitosis, and thus can control weeds as they germinate.
USP1-IN-6 (compound 11) is a USP1 inhibitor (IC50<50 nM). USP1-IN-5 also inhibits MDA-MB-436 cells with IC50 <50 nM[1].